Maximizing synthetic efficiency: Multi-component transformations lead the way

With the emergence of high-throughput screening in the pharmaceutical indus try in the early 1990's, organic chemists were faced with a new challenge: how to prepare large collections of molecules (the libraries) to "feed" the high-throughput screen? The unique exploratory power of some reactions (su ch as the 40 year-old Ugi four-component condensation) was soon recognized to be extremely valuable to produce Libraries in a time- and cost-effective manner. Over the last five years, industrial and academic researchers have made these powerful transformations into one of the most efficient and cos t-effective tools for combinatorial and parallel synthesis.